α-葡萄糖苷酶抑制剂固定化酶模型的建立及其对孔雀草不同组.PDFVIP

·2776 · 现代药物与临床 Drugs Clinic 第 33 卷 第 11 期 2018 年 11 月 α-葡萄糖苷酶抑制剂固定化酶模型的建立及其对孔雀草不同组分的筛选 朱连连，栾晓宁，窦德强* 辽宁中医药大学 药学院，辽宁 大连 116600 摘 要：目的 建立筛选 α-葡萄糖苷酶抑制剂的固定化酶筛选模型，进行孔雀草中活性组分的筛选研究。方法 采用共价 交联法固定 α-葡萄糖苷酶，模拟其在体内小肠壁上的情况，建立固定化酶筛选模型。使用 α-葡萄糖苷酶抑制剂阿卡波糖对 该模型进行验证。然后用该筛选模型对孔雀草 4 种提取组分进行筛选。结果 固定化酶的筛选模型更稳定，且可重复利用。 孔雀草水煎液和上清液组分对 α-葡萄糖苷酶的抑制率最强，醇沉组分次之，挥发油组分几乎无抑制作用。结论 该筛选模 型能很好地进行中药体外 α-葡萄糖苷酶抑制剂的筛选。 关键词：固定化酶；α-葡萄糖苷酶抑制剂；孔雀草；筛选 中图分类号：R965.1 文献标志码：A 文章编号：1674 - 5515(2018)11 - 2776 - 05 DOI: 10.7501/j.issn.1674-5515.2018.11.003 Establishment of an immobilized enzyme model for α-glucosidase inhibitor and screening on the compositions in Tagetes patula ZHU Lian-lian, LUAN Xiao-ning, DOU De-qiang College of Pharmacy, Liaoning University of Traditional Chinese Medicine, Dalian 116600, China Abstract: Objective To establish a screening model of immobilized enzymes for α-glucosidase inhibitors, and study the activities of the compositions in Tagetes patula. Methods Immobilization of α-glucosidase by covalent crosslinking was carried out, the situation on the intestinal membrane in vivo was simulated, and a screening model for α-glucosidase inhibitors was established. The model was validated by means of a standard α-glucosidase inhibitor acarbose. The model was used to screen the α-glucosidase inhibitors from four kinds of extract components in T. patula. Results The immobilized enzyme screening model was more stable, and could be reused. Water solution and the supernatant fluid composition in T. patula had the strongest inhibition for α-glucosidase enzymes, and then followed by alcohol precipitation components, but volatile oil components almost had no inhibition. Conclusion The screening model can be used for screening of α-glucosidase inhibitors for traditional Chinese medicine in vitro. Key words: immobilized enzyme; α-glu